139988-35-5

Upstream product

• 139988-95-7 1,2,5,6-tetrahydro-3-methyl-1-oxobenzo[f]quinazoline 
• 13726-52-8 diethyl N-(p-aminobenzoyl)-L-glutamate 
• 139987-91-0 1,2,5,6-tetrahydro-3-methyl-1-oxobenzo[f]-quinazolin-9-sulfonyl chloride 

Downstream Products

• 139988-37-7 diethyl N-<4-(1,2-dihydro-3-methyl-1-oxobenzoquinazoline-9-sulfonamido)benzoyl>-L-glutamate 

Relevant academic research and scientific papers

Combination of benzoquinazoline antifolates and protecting agents

The use of a protecting agent, for example a folate derivative such as folic acid or leucovorin, in combination with a non-competitive folic acid analogue, for example benzoquinazoline derivatives, for use in reducing the side effects associated with the

Pharmaceutically active benzoquinazoline compounds

Compounds of formula (I) or salts thereof, wherein the dotted line represents a single or double bond, R1is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4and R5are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8wherein n is the integer 0, 1 or 2 and R8is halo or alkyl or a group NR9R10wherein R9and R10are both hydrogen, a group NR11R12wherein R11and R12are the same or different and each is hydrogen or alkyl, a group OR13wherein R13is hydrogen or C1-4alkyl optionally substituted by halo; a C1-4aliphatic group optionally substituted by a group OR14or NR14R15wherein R14and R15are the same or different and each is hydrogen or alkyl; or two of R2to R5are linked together to form a benzo group, or one of R2to R5is a group -X-Y-R16wherein X is CH2, NR17, CO or S(O)m, and Y is CH2, NR17, O, or S(O)m, or -X-Y- is a group -O-, -NR17-, -CH=CH- or -N=N-, are disclosed as pharmacological agents useful in the treatment of tumours. Pharmaceutical compositions and methods for the preparation of compounds of formula (I) are also described.

PHARMACEUTICAL COMPOUNDS

The present invention relates to novel benzoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine

Benzoquinazoline Inhibitors of Thymidylate Synthase: Enzyme Inhibitory Activity and Cytotoxicity of Some Sulfonamidobenzoylglutamate and Related Derivatives

Several folate-like thymidylate synthase inhibitors are described in which the pteridine nucleus of the folic acid molecule is replaced by a benzoquinazoline moiety, which in turn is attached to the benzoylglutamate side chain by a sulfonamide link.The mo